A General Approach to the Synthesis of Polyamine Linked-Monoindolylmaleimides, a New Series of Trypanothione Reductase Inhibitors
| Autor: | Valérie Landry, Elisabeth Davioud-Charvet, Laurence Salmon, Louis Maes, Oleg Melnyk, Christian Sergheraert |
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| Rok vydání: | 1998 |
| Předmět: |
Trypanosoma
Indoles Stereochemistry Trypanosoma brucei Chemical synthesis Maleimides chemistry.chemical_compound Drug Discovery Polyamines Animals NADH NADPH Oxidoreductases Enzyme Inhibitors Trypanosoma cruzi Imide chemistry.chemical_classification biology Bicyclic molecule General Chemistry General Medicine biology.organism_classification Enzyme chemistry Biochemistry Enzyme inhibitor biology.protein Polyamine |
| Zdroj: | ResearcherID Chemical and pharmaceutical bulletin |
| ISSN: | 1347-5223 0009-2363 |
| DOI: | 10.1248/cpb.46.707 |
| Popis: | A simplified approach to the synthesis of 2-polyamine linked-monoindolylmaleimides has been achieved, leading to a new series of trypanothione reductase inhibitors. The conditions of access to N, 2-bis(polyamine)-3-monoindolylmaleimides and N, N'-bis(monoindolylmaleimide) polyamines are described. Measured inhibitory activities towards trypanothione reductase from Tryanosoma cruzi show the importance of both aromatic moieties and polyamine chains for trypanothione reductase recognition. |
| Databáze: | OpenAIRE |
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